An article 1,3-Dipolar Cycloaddition, HPLC Enantioseparation, and Docking Studies of Saccharin/Isoxazole and Saccharin/Isoxazoline Derivatives as Selective Carbonic Anhydrase IX and XII Inhibitors WOS:000526403900042 published article about SUBSTITUTED SACCHARIN DERIVATIVES; SECONDARY SULFONAMIDES; IN-VITRO; CANCER; ISOFORM; SCAFFOLD; POTENT; MODEL in [D’Ascenzio, Melissa; Secci, Daniela; Guglielmi, Paolo; Pierini, Marco] Sapienza Univ Rome, Dipartimento Chim & Tecnol Farmaco, I-00185 Rome, Italy; [Carradori, Simone; Zara, Susi] G dAnnunzio Univ Chieti Pescara, Dept Pharm, Via Vestini 31, I-66100 Chieti, Italy; [Cirilli, Roberto] Ist Super Sanita, Ctr Nazl Controllo & Valutaz Farm, I-00161 Rome, Italy; [Poli, Giulio; Tuccinardi, Tiziano] Univ Pisa, Dept Pharm, I-56126 Pisa, Italy; [Angeli, Andrea; Supuran, Claudiu T.] Univ Florence, Neurofarba Dept, Sect Pharmaceut & Nutraceut Sci, I-50019 Florence, Italy; [Angeli, Andrea] Petru Poni Inst Macromol Chem, Ctr Adv Res Bionanoconjugates, Iasi 700487, Romania; [Angeli, Andrea] Petru Poni Inst Macromol Chem, Biopolymers Dept, Iasi 700487, Romania in 2020.0, Cited 44.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Recommanded Product: 3-Pyridinecarboxaldehyde
Two series of saccharin/isoxazole and saccharin/isoxazoline hybrids were synthesized by 1,3-dipolar cycloaddition. The new compounds showed to be endowed with potent and selective inhibitory activity against the cancer-related human carbonic anhydrase (hCA) IX and XII isoforms in the nanomolar range, while no affinity was encountered for off-targets, such as hCA I and II. Successive enantioseparation on a milligram scale of the most representative compounds led to the discovery that (S)-isomers were more potent than their corresponding (R)-enantiomers. Lastly, molecular modeling studies were conducted to define those structural requirements that were responsible for the discrimination among selected human isoforms of carbonic anhydrases. Two nanomolar hCA IX and XII inhibitors were also screened for their selective toxicity against non tumoral primary cells (fibroblasts) and against a breast adenocarcinoma cell line (MCF7) in hypoxic environment. The efficacious combination of these compounds with doxorubicin on MCF7 cells was demonstrated after 72 h of treatment.
Recommanded Product: 3-Pyridinecarboxaldehyde. Welcome to talk about 500-22-1, If you have any questions, you can contact D’Ascenzio, M; Secci, D; Carradori, S; Zara, S; Guglielmi, P; Cirilli, R; Pierini, M; Poli, G; Tuccinardi, T; Angeli, A; Supuran, CT or send Email.
Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem